CN102415992A - Escitalopram oral liquid preparation - Google Patents
Escitalopram oral liquid preparation Download PDFInfo
- Publication number
- CN102415992A CN102415992A CN2011103781324A CN201110378132A CN102415992A CN 102415992 A CN102415992 A CN 102415992A CN 2011103781324 A CN2011103781324 A CN 2011103781324A CN 201110378132 A CN201110378132 A CN 201110378132A CN 102415992 A CN102415992 A CN 102415992A
- Authority
- CN
- China
- Prior art keywords
- escitalopram
- oral liquid
- antiseptic
- glycerol
- acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention discloses an escitalopram oral liquid preparation, comprising escitalopram and a PH adjusting agent with effective dosage. The pH value of the liquid is 4.0-5.2; and an acid buffering agent of the preferred malic acid-sodium citrate and citric acid-sodium citrate is the PH adjusting agent. The escitalopram oral liquid preparation also comprises a sweetening agent and a preservative. In the escitalopram oral liquid preparation, the stability is good, the escitalopram is difficultly degraded in water, the taste is good and the administration compliance is good.
Description
Technical field
The present invention relates to the escitalopram preparation, be specifically related to a kind of escitalopram oral liquid.
Background technology
The chemical name of escitalopram: (+)-1S-[3-(dimethylamino) propyl group]-1-(4-fluorophenyl)-1, the different phenylpropyl alcohol furan of 3-dihydro-5-nitrile oxalates, its structural formula is:
Molecular formula: C
20H
21FN
2OC
2H
2O
4
Molecular weight: 414.43
Escitalopram is mainly used in the treatment of depression clinically, has only tablet listing at present at home, because these article hydrolytically unstable and bitter in the mouth in liquid have easily limited its application in oral liquid.
Summary of the invention
The object of the present invention is to provide a kind of good stability, escitalopram oral liquid that mouthfeel is good.
The present invention realizes through following technical scheme:
A kind of oral liquid comprises the escitalopram of effective dose, it is characterized in that also comprising the PH regulator, and the pH value of said oral liquid is 4.0-5.2.
The preferred pH value of the present invention is 4.6.
Said PH regulator is acidic materials such as pharmaceutically useful hydrochloric acid, acetic acid, oxalic acid, phosphoric acid, malic acid, citric acid, acid buffer agent.
The preferred PH regulator of the present invention is an acid buffer agent.
Further, acid buffer agent preferred mass ratio of the present invention is citric acid and the sodium citrate that 6: 7 malic acid and sodium citrate or mass ratio is 1: 2.
Oral liquid of the present invention also comprises at least a pharmaceutically useful sweeting agent, like sucrose, glucose, fructose, maltose, lactose, mannitol, sorbitol, glycerol, propylene glycol and glucide, aspartame, acesulfame potassium, sucralose etc.
Preferred sweeteners of the present invention comprises at least a in glycerol, the propylene glycol.Like independent employing glycerol or propylene glycol as sweeting agent; Perhaps make up glycerol and sucrose as sweeting agent; Perhaps make up glycerol and aspartame as sweeting agent, perhaps make up glycerol and sucrose, maltose as sweeting agent, perhaps make up propylene glycol and mannitol as sweeting agent; Perhaps propylene glycol and glycerol, sorbitol combination as sweeting agent etc., as long as contain glycerol and/or propylene glycol in the sweeting agent.
Glycerol and/or propylene glycol are that concentration with 100-550ml/L exists in the above-mentioned sweeting agent.
Oral liquid of the present invention also comprises at least a antiseptic, and said antiseptic is selected from methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben, butoben, sodium benzoate.
Said antiseptic is that the concentration with 0.9-4.4g/L exists.
During preparation, escitalopram, PH regulator, antiseptic, sweeting agent are dissolved in the water by concentration requirement, stir and make dissolving and mix homogeneously fully, filter, embedding, sterilization promptly get.In order to make oral liquid mouthfeel of the present invention better, can also add an amount of aromatic, like Herba Menthae essence, Fructus Citri Limoniae essence, flavoring orange essence etc.
Beneficial effect of the present invention has:
(1) the pH stabilizing agent among the present invention can reduce the hydrolysis rate of escitalopram in liquid, and escitalopram can be degraded before the deadline, thereby guarantees the curative effect of medicine, prolongs the effect duration of product;
(2) adopt sweeting agent of the present invention, can cover the bitterness of escitalopram, improve the mouthfeel of preparation, improve the compliance of taking medicine;
(3) glycerol, propylene glycol are not only a kind of sweeting agent, also are cosolvent (cosolvent) and thickening agent simultaneously, and the effect that improves the preparation mouthfeel is not only arranged, and the dissolubility of the escitalopram of raising in water also arranged simultaneously and make the more stable effect of liquid preparation.Therefore multiple effect has been played in glycerol, propylene glycol use in the present invention, has obtained unexpected technique effect.
(4) use of antiseptic can make oral liquid of the present invention should not grow antibacterial, guarantees drug safety.
The specific embodiment
Embodiment 1
A kind of escitalopram oral liquid, contain following composition:
Method for preparing is: ethyl hydroxybenzoate is dissolved in an amount of glycerol, escitalopram, citric acid are dissolved in the suitable quantity of water, be stirred to dissolving fully; Add the glycerite of ethyl hydroxybenzoate, stir, add the glycerol of surplus; Add Herba Menthae essence, add water to 1000ml, mix homogeneously; Filter, embedding, sterilization promptly get.
Escitalopram oral liquid pH value of the present invention is 4.6.
The taking dose of escitalopram oral liquid of the present invention is each oral 5ml, contains escitalopram 5mg, and take 2-3 every day.
Embodiment 2
A kind of escitalopram oral liquid, contain following composition:
Method for preparing is: methyl hydroxybenzoate, propylparaben are dissolved in the propylene glycol, with escitalopram, citric acid, sodium citrate, add an amount of water stirring and dissolving; Add the propylene glycol solution of sorbitol and methyl hydroxybenzoate, propylparaben, stir, add flavoring orange essence; Add water to 1000ml; Stir, filter, embedding, sterilization promptly get.
Escitalopram oral liquid pH value of the present invention is 4.6.
Embodiment 3
A kind of escitalopram oral liquid, contain following composition:
Method for preparing is: ethyl hydroxybenzoate, butoben are dissolved in the propylene glycol, escitalopram, malic acid, sodium citrate are added stirring and dissolving in an amount of water, add the propylene glycol solution of glycerol and ethyl hydroxybenzoate, butoben; Stir; Add Fructus Citri Limoniae essence, add water to 1000ml, stir; Filter, embedding, sterilization promptly get.
Escitalopram oral liquid pH value of the present invention is 4.6.
Embodiment 4
A kind of escitalopram oral liquid, contain following composition:
Method for preparing is: ethyl hydroxybenzoate is dissolved in the glycerol, with escitalopram, malic acid, sodium citrate, sodium benzoate, adds an amount of water stirring and dissolving; Add the glycerite of sorbitol, ethyl hydroxybenzoate, stir, add Herba Menthae essence; Add water to 1000ml; Stir, filter, embedding, sterilization promptly get.
Escitalopram oral liquid pH value of the present invention is 4.6.
Embodiment 5
The screening test of PH regulator
(1) the 0.1g escitalopram is dissolved in 100ml water, gets Test Example 1
(2) respectively the 0.1g escitalopram is dissolved in 100ml water, regulates pH value to 3.6,4.0,4.5,5.2,5.5, get Test Example 2-6 with 0.1M hydrochloric acid;
(3) respectively the 0.1g escitalopram is dissolved in 100ml water, regulates pH value to 3.6,4.0,4.5,5.2,5.5, get Test Example 7-11 with citric acid;
(4) respectively the 0.1g escitalopram is dissolved in 100ml water, regulates pH value to 3.6,4.0,4.5,5.2,5.5, get Test Example 12-16 with malic acid-sodium citrate (6: 7) buffer agent;
(5) respectively the 0.1g escitalopram is dissolved in 100ml water, regulates pH value to 3.6,4.0,4.5,5.2,5.5, get Test Example 17-21 with citric acid-sodium citrate (1: 2) buffer agent.
(6) with above-mentioned 21 Test Example samples 60 ℃ hot environment held 10 days, surveyed pH value, content and related substance, result such as following table respectively at 0 day and 10 days:
Can find out from last table; The pH value of liquid preparation is on the rise; The content of escitalopram has the trend of reduction, and the content of related substance has the trend of increase, after adding the PH regulator; Above-mentioned trend is all slowed down to some extent, and the effect that wherein adds malic acid-sodium citrate (6: 7), citric acid-sodium citrate (1: 2) buffer agent obviously is superior to hydrochloric acid.Simultaneously can find out that also pH value solution when 4.0-5.2 is the most stable.
Claims (9)
1. escitalopram oral liquid is characterized in that comprising the escitalopram and the PH regulator of effective dose, and the pH value of said escitalopram oral liquid is 4.0-5.2.
2. escitalopram oral liquid as claimed in claim 1 is characterized in that pH value is 4.6.
3. according to claim 1 or claim 2 escitalopram oral liquid is characterized in that said PH regulator is an acid buffer agent.
4. escitalopram oral liquid as claimed in claim 3 is characterized in that said acid buffer agent is that mass ratio is citric acid and the sodium citrate that 6: 7 malic acid and sodium citrate or mass ratio is 1: 2.
5. according to claim 1 or claim 2 escitalopram oral liquid is characterized in that also comprising at least a pharmaceutically useful sweeting agent.
6. escitalopram oral liquid as claimed in claim 5 is characterized in that said sweeting agent comprises at least a in glycerol, the propylene glycol.
7. escitalopram oral liquid as claimed in claim 6 is characterized in that said glycerol and/or propylene glycol are that concentration with 100-550ml/L exists.
8. according to claim 1 or claim 2 escitalopram oral liquid; It is characterized in that also comprising antiseptic; Said antiseptic is one or more combination of methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben, butoben, sodium benzoate, and said antiseptic is that the concentration with 0.9-4.4g/L exists.
9. escitalopram oral liquid as claimed in claim 5; It is characterized in that also comprising antiseptic; Said antiseptic is one or more combination of methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben, butoben, sodium benzoate, and said antiseptic is that the concentration with 0.9-4.4g/L exists.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011103781324A CN102415992A (en) | 2011-11-24 | 2011-11-24 | Escitalopram oral liquid preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011103781324A CN102415992A (en) | 2011-11-24 | 2011-11-24 | Escitalopram oral liquid preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102415992A true CN102415992A (en) | 2012-04-18 |
Family
ID=45940796
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011103781324A Pending CN102415992A (en) | 2011-11-24 | 2011-11-24 | Escitalopram oral liquid preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102415992A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106491521A (en) * | 2016-09-22 | 2017-03-15 | 北京万全德众医药生物技术有限公司 | A kind of oral liquor of escitalopram oxalate |
| CN110787304A (en) * | 2018-08-02 | 2020-02-14 | 北京万全德众医药生物技术有限公司 | Preparation method of escitalopram oxalate clathrate oral liquid |
| KR20200119021A (en) * | 2019-04-09 | 2020-10-19 | 주식회사 라이트팜텍 | Oral solution composition containing escitalopram with good stability and the method for preparing the same |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1726298A2 (en) * | 2005-05-05 | 2006-11-29 | Errekappa Euroterapici S.p.A. | Oral liquid formulations containing citalopram |
| CN1911207A (en) * | 2006-09-08 | 2007-02-14 | 上海实业联合集团长城药业有限公司 | Oral liquor contg. citalopram hydrobromide and its prepn. method |
| CN101313903A (en) * | 2007-06-01 | 2008-12-03 | 北京德众万全药物技术开发有限公司 | Medicament composition containing escitalopram |
-
2011
- 2011-11-24 CN CN2011103781324A patent/CN102415992A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1726298A2 (en) * | 2005-05-05 | 2006-11-29 | Errekappa Euroterapici S.p.A. | Oral liquid formulations containing citalopram |
| CN1911207A (en) * | 2006-09-08 | 2007-02-14 | 上海实业联合集团长城药业有限公司 | Oral liquor contg. citalopram hydrobromide and its prepn. method |
| CN101313903A (en) * | 2007-06-01 | 2008-12-03 | 北京德众万全药物技术开发有限公司 | Medicament composition containing escitalopram |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106491521A (en) * | 2016-09-22 | 2017-03-15 | 北京万全德众医药生物技术有限公司 | A kind of oral liquor of escitalopram oxalate |
| CN110787304A (en) * | 2018-08-02 | 2020-02-14 | 北京万全德众医药生物技术有限公司 | Preparation method of escitalopram oxalate clathrate oral liquid |
| KR20200119021A (en) * | 2019-04-09 | 2020-10-19 | 주식회사 라이트팜텍 | Oral solution composition containing escitalopram with good stability and the method for preparing the same |
| KR102331187B1 (en) * | 2019-04-09 | 2021-11-26 | 주식회사 라이트팜텍 | Oral solution composition containing escitalopram with good stability and the method for preparing the same |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP4445590B2 (en) | Oral liquid composition containing paroxetine-resin | |
| CN102046180A (en) | Compositions and methods for immunotherapy | |
| KR100841893B1 (en) | Pregabalin Composition | |
| CN102743333A (en) | Levetiracetam oral liquid and preparation method of levetiracetam oral liquid | |
| CN102415992A (en) | Escitalopram oral liquid preparation | |
| WO2011160425A1 (en) | Preparing method of allicin injection and low temperature continuous stirring ultrafiltration device thereof | |
| WO2005004874A1 (en) | Stable tetrodotoxin freeze drying medicinal preparation | |
| JP4959335B2 (en) | Methylphenidate solution and related administration and manufacturing methods | |
| CN1259910C (en) | Liquid drug preparations | |
| EP2934593B1 (en) | Cabazitaxel composition | |
| JP6410814B2 (en) | Liquid pharmaceutical composition for oral administration containing fexofenadine | |
| CN106619502A (en) | Levetiracetam oral solution and preparation method thereof | |
| CN100406021C (en) | Breviscapine B injection preparation and its preparing method | |
| WO2014071743A1 (en) | Composition containing antifungal drug and lactate buffer | |
| CN103830240B (en) | A kind of flouroquinolone drugs compositions | |
| WO2011127537A1 (en) | Radiation sensitiser compositions | |
| CN101822822A (en) | Drug composition of pramlintide and preparation method thereof | |
| CN1867325A (en) | Jelly pharmaceutical preparation containing biguanide-based medicine | |
| CN102370656A (en) | Clarithromycin medicine composition and preparation method thereof | |
| TWI449704B (en) | Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same | |
| TW201004656A (en) | A stable fluid composition of taxane derivatives, preparing method and use thereof | |
| KR20120031051A (en) | Oral liquid preparation | |
| CN107510650B (en) | Pidotimod oral solution and preparation method thereof | |
| WO2009103209A1 (en) | Stable s-(-)- nadifloxacin-l-arginine composition, its preparation method and use | |
| JP2010516717A (en) | Oxaliplatin pharmaceutical composition with alcoholic sugar-based buffer |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C53 | Correction of patent of invention or patent application | ||
| CB02 | Change of applicant information |
Address after: 430056, No. three, No. 9, Maple Road, Wuhan economic and Technological Development Zone, Hubei, Wuhan Applicant after: Ferguson (Wuhan) Biological Technology Co., Ltd. Address before: 430056, building 8, hi tech Industrial Park, Wuhan economic and Technological Development Zone, Wuhan, Hubei Applicant before: Ferguson (Wuhan) Biological Technology Co., Ltd. |
|
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20120418 |